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Ciprofloxacin‐isatin‐1 H ‐1,2,3‐triazole Hybrids: Design, Synthesis, and in vitro Anti‐tubercular Activity against M . tuberculosis
Author(s) -
Xu Zhi,
Lv ZaoSheng,
Song XuFeng,
Qiang Min
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3010
Subject(s) - chemistry , cytotoxicity , isatin , vero cell , ciprofloxacin , in vitro , mycobacterium tuberculosis , conjugate , triazole , minimum inhibitory concentration , microbiology and biotechnology , stereochemistry , tuberculosis , biochemistry , antibiotics , biology , organic chemistry , medicine , mathematical analysis , mathematics , pathology
A new set of ciprofloxacin (CPFX)‐isatin‐1 H ‐1,2,3‐triazole hybrids 6a – l with greater lipophilicity compared with the parent CPFX was designed, synthesized, and assessed for their in vitro anti‐mycobacterial activity against Mycobacterium tuberculosis (MTB) H 37 Rv as well as cytotoxicity in VERO cell line. The preliminary results showed that all hybrids (MIC: 0.39–50 μg/mL) exhibited promising activities against MTB H 37 Rv, and six of them (MIC: 0.39–1.56 μg/mL) were more active than the parent CPFX (MIC: 3.12 μg/mL). In particular, the most active conjugate 6h (MIC: 0.39 μg/mL) was comparable with RIF (MIC: 0.39 μg/mL), and eight times more potent than CPFX. All conjugates (CC 50 : 4–64 μg/mL) were more toxic than the parent (CC 50 : 128 μg/mL) in VERO cell lines, and the most active hybrids, which also displayed the highest cytotoxicity, should be further optimized.